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Assay Detail

CHEMBL765807

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibitory activity determined against prolyl oligopeptidase (Tc80) in Trypanosoma cruzi
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.
Bal G, Van der Veken P, Antonov D, Lambeir AM, Grellier P, Croft SL, Augustyns K, Haemers A.
Bioorg Med Chem Lett (2003) 13 : 2875 -2878
PubMed 14611847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.84 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97152 2 9.68
CHEMBL95698 1 9.59
CHEMBL318284 3 9.55
CHEMBL99305 1 9.35
CHEMBL100213 1 8.12
CHEMBL99237 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97152 Ki = 0.21 nM 9.68
CHEMBL95698 Ki = 0.26 nM 9.59
CHEMBL318284 Ki = 0.28 nM 9.55
CHEMBL99305 Ki = 0.45 nM 9.35
CHEMBL318284 Ki = 1.25 nM 8.90
CHEMBL97152 Ki = 1.87 nM 8.73
CHEMBL318284 Ki = 3.3 nM 8.48
CHEMBL100213 Ki = 7.5 nM 8.12
CHEMBL99237 Ki = 72.0 nM 7.14